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Novel DPP-IV inhibitors

A technology of excipient and diluent, applied in the field of novel DPP-IV inhibitors, can solve the problem that the physiological role of DPP-IV has not been fully elucidated

Active Publication Date: 2015-11-25
DNJ PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The physiological role of DPP-IV has not been fully elucidated

Method used

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Embodiment Construction

[0020] The present invention provides novel inhibitors of dipeptidyl peptidase IV with other activities such as β-receptor blocker activity, which include modified N-substituted pyrrolidine compounds of the following general formula (I):

[0021]

[0022] Formula I

[0023] wherein the pyrrolidine ring formed by X, Z, N and the carbon atoms to which they are attached is saturated or optionally contains a double bond;

[0024] A can be H, F or CN;

[0025] X is selected from CH 2 , CH, S, O, NH, N, C=O, CF 2 , CF, CH-Y and C-Y, wherein Y is halogen, hydroxyl or C1-C3 alkoxy;

[0026] Z is selected from CH 2 , CH, CF 2 , CF, C-Y and CH-Y;

[0027] One of X or Z must be CH 2 ; or CH, if the pyrrolidine ring contains a double bond; wherein G is:

[0028]

[0029] wherein M, Q and V represent carbon atoms;

[0030] n is 0 or 1; and

[0031] where R 1 and R 2 Connect with V and Q, or R 2 and R 3 Together with Q and M, a 3-6 membered saturated carbocyclic or heteroc...

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Abstract

The invention comprises novel inhibitors of dipeptidyl peptidase IV (DPP-IV) with beta blocker activity, pharmaceutical compositions comprising therapeutically effective amounts of novel inhibitors of DPP-IV, and novel methods of treating medical conditions are provided. The novel inhibitors of DPP-IV described herein are useful in the treatment of neurological disorders, diabetes, inflammatory disorders such as arthritis, obesity, osteoporosis, hypertension, and glaucoma of such other enumerated conditions as can be treated with inhibitors of DPP-IV and beta blockers.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to U.S. Utility Patent Application No. 13 / 744,795, filed January 8, 2013, which claims priority to U.S. Provisional Patent Application No. 61 / 587,826, filed January 18, 2012, which The disclosure content is incorporated into this application by reference. technical field [0003] The present invention relates to new and improved inhibitors of dipeptidyl peptidase IV (DPP-IV) having beta receptor blocker activity as well as new and improved methods of treatment and related uses. Inhibitors according to the invention are useful in the treatment and detection of various diseases and other abnormal states, including diseases affecting the central nervous system. Background technique [0004] Dipeptidyl peptidase-IV (DPP-IV, EC 3.4.14.5) is a protein encoded by the DPP4 gene in humans. This protein is an antigenic enzyme expressed on the surface of most types of cells and is involved in im...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/16C07D401/06C07D413/06C07D417/06A61K31/40A61K31/404A61P9/00A61P25/00
CPCC07D207/16A61K31/40C07D295/185C07D295/192A61P25/00A61P9/00
Inventor 凯瑟琳·F·杨李卫星
Owner DNJ PHARMA
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